iclaprim profile

iclaprim: has antiviral activity [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

iclaprim : A racemate consisting of equimolar amounts of (R)- and (S)-iclaprim. Both enantiomers exhibit similar, potent bactericidal activity against major Gram-positive pathogens, notably methicillin-sensitive and -resistant Staphylococcus aureus (MSSA and MRSA, respectively). [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

5-[(2-cyclopropyl-7,8-dimethoxy-2H-chromen-5-yl)methyl]pyrimidine-2,4-diamine : An aminopyrimidine that is 5-methylpyrimidine-2,4-diamine in which one of the hydrogens of the methyl group has been replaced by a 2-cyclopropyl-7,8-dimethoxy-2H-chromen-5-yl group. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

ID Source	ID
PubMed CID	213043
CHEMBL ID	134561
CHEBI ID	131751
SCHEMBL ID	379386
SCHEMBL ID	12899446
MeSH ID	M0466801

Synonym
mersarex
iclaprim
ar-100
2,4-pyrimidinediamine, 5-[(2-cyclopropyl-7,8-dimethoxy-2h-1-benzopyran-5-yl)methyl]-
192314-93-5
5-[(2-cyclopropyl-7,8-dimethoxy-2h-chromen-5-yl)methyl]pyrimidine-2,4-diamine
ro-48-2622
bdbm18070
ro-482622
CHEMBL134561
ro 48-2622
iclaprim (usan/inn)
D08337
CHEBI:131751
iclaprim [usan:inn]
5-((2rs)-2-cyclopropyl-7,8-dimethoxy-2h-chromen-5-ylmethyl)pyrimidine-2,4-diamine
2,4-pyrimidinediamine, 5-((2-cyclopropyl-7,8-dimethoxy-2h-1-benzopyran-5-yl)methyl)-
unii-42445huu0o
ar 100
42445huu0o ,
FT-0670271
FT-0670272
iclaprim [who-dd]
iclaprim [usan]
iclaprim [mi]
iclaprim [inn]
5-{[(2rs)-2-cyclopropyl-7,8-dimethoxy-2h-1-benzopyran-5-yl]methyl}pyrimidine-2,4-diamine
iclaprim [mart.]
SCHEMBL379386
SCHEMBL12899446
5-(2-cyclopropyl-7,8-dimethoxy-2h-chromen-5-ylmethyl)-pyrimidine-2,4-diamine (iclaprim]
5-[(2-cyclopropyl-7,8-dimethoxy-2h-1-benzopyran-5-yl)methyl]-2,4-pyrimidine- diamine
AKOS027422438
AS-74032
W16646
J-012427
CS-7873
HY-101479
5-[(2-cyclopropyl-7,8-dimethoxy-2h-chromen-5-yl)methyl]pyrimidine-2,4- diamine
BCP04499
DTXSID70870191
5-[(2-cyclopropyl-7,8-dimethoxy-2h-1-benzopyran-5-yl)methyl]pyrimidine-2,4-diamine
5-((2-cyclopropyl-7,8-dimethoxy-2h-chromen-5-yl)methyl)pyrimidine-2,4-diamine
mfcd09837803
DB06358
Q907480
SB17354
HMS3749A21
ro 63-9141;bal 9141
gtpl10820
ar-100ar-100

Excerpt	Reference	Relevance
"Iclaprim is a novel diaminopyrimidine antibiotic that is active against methicillin-resistant Staphylococcus aureus (MRSA). "	( Efficacy of iclaprim against wild-type and thymidine kinase-deficient methicillin-resistant Staphylococcus aureus isolates in an in vitro fibrin clot model. Entenza, JM; Giddey, M; Haldimann, A; Hawser, S; Lociuro, S; Moreillon, P, 2009)	2.17
"Iclaprim is a novel diaminopyrimidine antibiotic that may be an effective and safe treatment for serious skin infections. "	( A Phase 3, Randomized, Double-Blind, Multicenter Study To Evaluate the Safety and Efficacy of Intravenous Iclaprim versus Vancomycin for Treatment of Acute Bacterial Skin and Skin Structure Infections Suspected or Confirmed To Be Due to Gram-Positive Path Borghei, A; Corey, GR; Dryden, M; File, TM; Holland, TL; Huang, DB; Lodise, T; McLeroth, P; McManus, A; O'Riordan, W; Oguri, T; Shin, E; Shukla, R; Torres, A; Wilcox, MH, 2018)	2.14
"Iclaprim is an antibiotic under development for the treatment of patients with acute bacterial skin and skin structure infections and is not associated with acute kidney injury."	( Potential for Cost Saving with Iclaprim Owing to Avoidance of Vancomycin-Associated Acute Kidney Injury in Hospitalized Patients with Acute Bacterial Skin and Skin Structure Infections. Huang, D; Lodise, T; Patel, N, 2018)	1.49
"Iclaprim is a selective bacterial dihydrofolate reductase (DHFR) inhibitor. "	( Iclaprim: a differentiated option for the treatment of skin and skin structure infections. Corey, GR; Huang, DB; Noviello, S, 2018)	3.37
"Iclaprim is a dihydrofolate reductase inhibitor with greatly enhanced activity, as compared with trimethoprim, against a range of Gram-positive and Gram-negative pathogens."	( What's new and not so new on the antimicrobial horizon? French, GL, 2008)	1.07
"Iclaprim is a novel 2,4-diaminopyrimidine that exhibits potent, rapid bactericidal activity against major Gram-positive pathogens, including methicillin-susceptible Staphylococcus aureus and methicillin-resistant S. "	( Increased hydrophobic interactions of iclaprim with Staphylococcus aureus dihydrofolate reductase are responsible for the increase in affinity and antibacterial activity. Bandera, M; Dale, GE; Haldimann, A; Laue, H; Lociuro, S; Mukhija, S; Oefner, C; Parisi, S; Schulz, H; Weiss, L, 2009)	2.07
"Iclaprim is a novel diaminopyrimidine currently in phase III clinical development. "	( In vitro activity of iclaprim and comparison agents tested against Neisseria gonorrhoeae including medium growth supplement effects. Biedenbach, DJ; Jones, RN; Sader, HS, 2009)	2.11
"Iclaprim is a novel antibacterial agent that is currently in development for the treatment of complicated skin and skin structure infections (cSSSI). "	( Multicenter, randomized study of the efficacy and safety of intravenous iclaprim in complicated skin and skin structure infections. Brandt, R; Hadvary, P; Hawser, S; Islam, K; Krievins, D, 2009)	2.03
"Iclaprim is a promising antimicrobial agent for the treatment of gram-positive organisms, including resistant S. "	( Iclaprim, a novel diaminopyrimidine for the treatment of resistant gram-positive infections. Schmidt, JM; Sincak, CA, 2009)	3.24
"Iclaprim is a novel dihydrofolate reductase (DHFR) inhibitor belonging to the 2,4-diaminopyrimidine class of antibiotics, of which trimethoprim (TMP) is the most well known representative. "	( Inhibitory properties and X-ray crystallographic study of the binding of AR-101, AR-102 and iclaprim in ternary complexes with NADPH and dihydrofolate reductase from Staphylococcus aureus. Dale, GE; Lociuro, S; Oefner, C; Parisi, S; Schulz, H, 2009)	2.02
"Iclaprim is a novel diaminopyrimidine, and an inhibitor of dihydrofolate reductase, which has shown potent, extended-spectrum in vitro activity against Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus, vancomycin-intermediate and vancomycin-resistant S. "	( Iclaprim. Kohlhoff, SA; Sharma, R, 2007)	3.23
"Iclaprim is a novel diaminopyrimidine for which a human plasma binding level of approximately 93% has been reported. "	( Effect of human plasma on the antimicrobial activity of iclaprim in vitro. Hawser, S; Islam, K; Laue, H; Lociuro, S; Seguin, A; Valensise, T, 2007)	2.03

Excerpt	Reference	Relevance
"Iclaprim has the potential to reduce the economic burden of acute bacterial skin and skin structure infections in hospitalized patients at risk for vancomycin-associated acute kidney injury when iclaprim acquisition is US$300/day or less."	( Potential for Cost Saving with Iclaprim Owing to Avoidance of Vancomycin-Associated Acute Kidney Injury in Hospitalized Patients with Acute Bacterial Skin and Skin Structure Infections. Huang, D; Lodise, T; Patel, N, 2018)	2.21

Excerpt	Reference	Relevance
"Iclaprim treatment duration was 7 days and iclaprim acquisition cost was varied to determine the upper end of the daily iclaprim price that still conferred cost savings relative to vancomycin."	( Potential for Cost Saving with Iclaprim Owing to Avoidance of Vancomycin-Associated Acute Kidney Injury in Hospitalized Patients with Acute Bacterial Skin and Skin Structure Infections. Huang, D; Lodise, T; Patel, N, 2018)	1.49

Excerpt	Reference	Relevance
" The adverse event profile of both iclaprim dosing regimens was similar to that of vancomycin."	( A Phase II Randomized, Double-blind, Multicenter Study to Evaluate Efficacy and Safety of Intravenous Iclaprim Versus Vancomycin for the Treatment of Nosocomial Pneumonia Suspected or Confirmed to be Due to Gram-positive Pathogens. Corey, GR; Dryden, M; File, TM; Hadvary, P; Huang, DB; Shorr, AF; Torres, A; Wilcox, MH, 2017)	0.95
" Iclaprim was well tolerated in the study, with most adverse events categorized as mild."	( A Phase 3, Randomized, Double-Blind, Multicenter Study to Evaluate the Safety and Efficacy of Intravenous Iclaprim Vs Vancomycin for the Treatment of Acute Bacterial Skin and Skin Structure Infections Suspected or Confirmed to be Due to Gram-Positive Path Amin, F; Corey, GR; Dryden, M; File, TM; Heller, B; Holland, TL; Huang, DB; McLeroth, P; O'Riordan, W; Overcash, JS; Shukla, R; Torres, A; Wilcox, MH, 2018)	1.6
" Based on these results, iclaprim appears to be an efficacious and safe treatment for ABSSSI suspected or confirmed to be due to gram-positive pathogens."	( A Phase 3, Randomized, Double-Blind, Multicenter Study to Evaluate the Safety and Efficacy of Intravenous Iclaprim Vs Vancomycin for the Treatment of Acute Bacterial Skin and Skin Structure Infections Suspected or Confirmed to be Due to Gram-Positive Path Amin, F; Corey, GR; Dryden, M; File, TM; Heller, B; Holland, TL; Huang, DB; McLeroth, P; O'Riordan, W; Overcash, JS; Shukla, R; Torres, A; Wilcox, MH, 2018)	1
"Iclaprim is a novel diaminopyrimidine antibiotic that may be an effective and safe treatment for serious skin infections."	( A Phase 3, Randomized, Double-Blind, Multicenter Study To Evaluate the Safety and Efficacy of Intravenous Iclaprim versus Vancomycin for Treatment of Acute Bacterial Skin and Skin Structure Infections Suspected or Confirmed To Be Due to Gram-Positive Path Borghei, A; Corey, GR; Dryden, M; File, TM; Holland, TL; Huang, DB; Lodise, T; McLeroth, P; McManus, A; O'Riordan, W; Oguri, T; Shin, E; Shukla, R; Torres, A; Wilcox, MH, 2018)	2.14
" Iclaprim and vancomycin were comparable for the incidence of mostly mild adverse events, except for a higher incidence of elevated serum creatinine with vancomycin (n = 7) compared with iclaprim (n = 0)."	( Pooled analysis of the phase 3 REVIVE trials: randomised, double-blind studies to evaluate the safety and efficacy of iclaprim versus vancomycin for treatment of acute bacterial skin and skin-structure infections. Balser, B; Corey, GR; Desplats, E; Dryden, M; File, TM; Holland, TL; Huang, DB; Lodise, T; O'Riordan, W; Torres, A; Wilcox, MH, 2018)	1.6
" The safety profile was assessed based on adverse events and laboratory parameters."	( A Pooled Analysis of the Safety and Efficacy of Iclaprim Versus Vancomycin for the Treatment of Acute Bacterial Skin and Skin Structure Infections in Patients With Intravenous Drug Use: Phase 3 REVIVE Studies. Balser, B; Corey, GR; Huang, DB; Noviello, S; Scaramucci, A, 2019)	0.77

Excerpt	Reference	Relevance
"To assess the synergistic potential of the novel diaminopyrimidine iclaprim (formerly AR-100, Ro 48-2622), a specific and selective inhibitor of microbial dihydrofolate reductase (DHFR), in combination with other antimicrobial agents with distinctly different mechanisms of action."	( In vitro activity of the novel diaminopyrimidine, iclaprim, in combination with folate inhibitors and other antimicrobials with different mechanisms of action. Bernardi, A; Hawser, S; Islam, K; Laue, H; Lociuro, S; Weiss, L, 2007)	0.83
"In chequerboard studies, iclaprim was tested in combination with 32 different antimicrobial agents against Gram-positive, Gram-negative and anaerobic bacteria including reference strains."	( In vitro activity of the novel diaminopyrimidine, iclaprim, in combination with folate inhibitors and other antimicrobials with different mechanisms of action. Bernardi, A; Hawser, S; Islam, K; Laue, H; Lociuro, S; Weiss, L, 2007)	0.9
" Furthermore, iclaprim exhibited no synergy or antagonism when evaluated in combination with metronidazole or aztreonam against a panel of 19 bacterial strains, including Gram-positive, Gram-negative and selected anaerobic bacteria."	( In vitro activity of the novel diaminopyrimidine, iclaprim, in combination with folate inhibitors and other antimicrobials with different mechanisms of action. Bernardi, A; Hawser, S; Islam, K; Laue, H; Lociuro, S; Weiss, L, 2007)	0.95
" Notably, iclaprim exhibited indifference in combination with aztreonam and metronidazole against Gram-negatives and anaerobes, respectively."	( In vitro activity of the novel diaminopyrimidine, iclaprim, in combination with folate inhibitors and other antimicrobials with different mechanisms of action. Bernardi, A; Hawser, S; Islam, K; Laue, H; Lociuro, S; Weiss, L, 2007)	1

Excerpt	Relevance	Reference
" The adverse event profile of both iclaprim dosing regimens was similar to that of vancomycin."	( A Phase II Randomized, Double-blind, Multicenter Study to Evaluate Efficacy and Safety of Intravenous Iclaprim Versus Vancomycin for the Treatment of Nosocomial Pneumonia Suspected or Confirmed to be Due to Gram-positive Pathogens. Corey, GR; Dryden, M; File, TM; Hadvary, P; Huang, DB; Shorr, AF; Torres, A; Wilcox, MH, 2017)	0.95

Class	Description
aminopyrimidine	A member of the class of pyrimidines that is pyrimidine substituted by at least one amino group and its derivatives.
chromenes
cyclopropanes	Cyclopropane and its derivatives formed by substitution.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Dihydrofolate reductase	Homo sapiens (human)	IC50 (µMol)	47.4900	0.0006	0.8726	7.3000	AID1797691; AID56158; AID56954
Dihydrofolate reductase	Homo sapiens (human)	Ki	0.7750	0.0000	0.3756	4.9000	AID1074586; AID614170
Dihydrofolate reductase	Staphylococcus aureus	IC50 (µMol)	33.6068	0.0022	0.1976	2.4000	AID1797691; AID55995; AID575154; AID575155
Dihydrofolate reductase	Staphylococcus aureus	Ki	0.0004	0.0001	0.1618	1.7290	AID1074587; AID614168; AID614173
Dihydrofolate reductase	Escherichia coli K-12	IC50 (µMol)	50.4048	0.0015	0.5512	6.8000	AID1797691; AID57238
Dihydrofolate reductase	Pneumocystis carinii	IC50 (µMol)	50.8037	0.0006	0.5476	6.2000	AID1797691; AID55685
Dihydrofolate reductase	Streptococcus pneumoniae TIGR4	IC50 (µMol)	60.4844	0.0070	0.3587	2.4000	AID1797691
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
tetrahydrobiopterin biosynthetic process	Dihydrofolate reductase	Homo sapiens (human)
one-carbon metabolic process	Dihydrofolate reductase	Homo sapiens (human)
negative regulation of translation	Dihydrofolate reductase	Homo sapiens (human)
axon regeneration	Dihydrofolate reductase	Homo sapiens (human)
response to methotrexate	Dihydrofolate reductase	Homo sapiens (human)
dihydrofolate metabolic process	Dihydrofolate reductase	Homo sapiens (human)
tetrahydrofolate metabolic process	Dihydrofolate reductase	Homo sapiens (human)
tetrahydrofolate biosynthetic process	Dihydrofolate reductase	Homo sapiens (human)
folic acid metabolic process	Dihydrofolate reductase	Homo sapiens (human)
positive regulation of nitric-oxide synthase activity	Dihydrofolate reductase	Homo sapiens (human)
regulation of removal of superoxide radicals	Dihydrofolate reductase	Homo sapiens (human)
10-formyltetrahydrofolate biosynthetic process	Dihydrofolate reductase	Escherichia coli K-12
response to xenobiotic stimulus	Dihydrofolate reductase	Escherichia coli K-12
folic acid biosynthetic process	Dihydrofolate reductase	Escherichia coli K-12
one-carbon metabolic process	Dihydrofolate reductase	Escherichia coli K-12
response to methotrexate	Dihydrofolate reductase	Escherichia coli K-12
tetrahydrofolate biosynthetic process	Dihydrofolate reductase	Escherichia coli K-12
response to antibiotic	Dihydrofolate reductase	Escherichia coli K-12
dihydrofolate metabolic process	Dihydrofolate reductase	Escherichia coli K-12
folic acid metabolic process	Dihydrofolate reductase	Escherichia coli K-12
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
mRNA regulatory element binding translation repressor activity	Dihydrofolate reductase	Homo sapiens (human)
mRNA binding	Dihydrofolate reductase	Homo sapiens (human)
dihydrofolate reductase activity	Dihydrofolate reductase	Homo sapiens (human)
folic acid binding	Dihydrofolate reductase	Homo sapiens (human)
NADPH binding	Dihydrofolate reductase	Homo sapiens (human)
sequence-specific mRNA binding	Dihydrofolate reductase	Homo sapiens (human)
NADP binding	Dihydrofolate reductase	Homo sapiens (human)
dihydrofolate reductase activity	Dihydrofolate reductase	Escherichia coli K-12
protein binding	Dihydrofolate reductase	Escherichia coli K-12
folic acid binding	Dihydrofolate reductase	Escherichia coli K-12
oxidoreductase activity	Dihydrofolate reductase	Escherichia coli K-12
NADP binding	Dihydrofolate reductase	Escherichia coli K-12
methotrexate binding	Dihydrofolate reductase	Escherichia coli K-12
dihydrofolic acid binding	Dihydrofolate reductase	Escherichia coli K-12
NADP+ binding	Dihydrofolate reductase	Escherichia coli K-12
NADPH binding	Dihydrofolate reductase	Escherichia coli K-12
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
mitochondrion	Dihydrofolate reductase	Homo sapiens (human)
cytosol	Dihydrofolate reductase	Homo sapiens (human)
mitochondrion	Dihydrofolate reductase	Homo sapiens (human)
cytosol	Dihydrofolate reductase	Escherichia coli K-12
cytosol	Dihydrofolate reductase	Escherichia coli K-12
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (205)

Assay ID	Title	Year	Journal	Article
AID556169	Drug concentration in epithelial lining fluid of patient with Streptococcus pneumoniae infections at 1.6 mg/kg, iv administered as single 60 mins infusion measured after 3 to 4 hrs	2009	Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4	In vitro activity of Iclaprim against respiratory and bacteremic isolates of Streptococcus pneumoniae.
AID561751	Antibacterial activity against Enterococcus faecium assessed as inhibition of bacterial growth at 0.12 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID561519	Antibacterial activity against Methicillin-sensitive Staphylococcus aureus assessed as inhibition of bacterial growth at 0.06 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID571554	Antimicrobial activity against methicillin-resistant Staphylococcus aureus AW6 grown on CAMHB media after 24 hrs by broth microdilution method in presence of protein depleted human serum	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	Efficacy of iclaprim against wild-type and thymidine kinase-deficient methicillin-resistant Staphylococcus aureus isolates in an in vitro fibrin clot model.
AID561553	Antibacterial activity against Beta-hemolytic Streptococcus group A assessed as inhibition of bacterial growth at 1 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID56158	Inhibition of Streptococcus pneumoniae dihydrofolate reductase (DHFR) enzyme by trimethoprim (TMP)	2003	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23	Iclaprim, a novel diaminopyrimidine with potent activity on trimethoprim sensitive and resistant bacteria.
AID561568	Antibacterial activity against Beta-hemolytic Streptococcus group B assessed as inhibition of bacterial growth at 2 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID565503	Ratio of MIC for glycopeptide-nonsusceptible Staphylococcus aureus NJ992 in presence of 50% heat inactivated serum to MIC for glycopeptide-nonsusceptible Staphylococcus aureus NJ992	2009	Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10	In vitro bactericidal activity of iclaprim in human plasma.
AID571778	Antimicrobial activity against thymidine kinase-deficient methicillin-resistant Staphylococcus aureus AH1252 grown on CAMHB media after 24 hrs by broth microdilution method in presence of 50% human serum and 1 ug/ml thymidine	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	Efficacy of iclaprim against wild-type and thymidine kinase-deficient methicillin-resistant Staphylococcus aureus isolates in an in vitro fibrin clot model.
AID206646	Antibacterial activity against methicillin resistant Staphylococcus aureus (MRSA)	2003	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23	Iclaprim, a novel diaminopyrimidine with potent activity on trimethoprim sensitive and resistant bacteria.
AID561540	Antibacterial activity against Methicillin-resistant Staphylococcus aureus assessed as inhibition of bacterial growth at 4 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID561722	Antibacterial activity against Enterococcus faecalis assessed as inhibition of bacterial growth at <= 0.008 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID571558	Antimicrobial activity against thymidine kinase-deficient methicillin-resistant Staphylococcus aureus AH1252 grown on CAMHB media after 24 hrs by broth microdilution method in presence of 50% rat serum and 0.2 U/ml thymidine phosphorylase	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	Efficacy of iclaprim against wild-type and thymidine kinase-deficient methicillin-resistant Staphylococcus aureus isolates in an in vitro fibrin clot model.
AID565486	Bactericidal activity against methicillin-resistant Staphylococcus aureus after 24 hrs by M26-A method in presence of 50% human plasma	2009	Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10	In vitro bactericidal activity of iclaprim in human plasma.
AID561548	Antibacterial activity against Beta-hemolytic Streptococcus group A assessed as inhibition of bacterial growth at 0.03 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID561532	Antibacterial activity against Methicillin-resistant Staphylococcus aureus assessed as inhibition of bacterial growth at 0.015 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID561541	Antibacterial activity against Methicillin-resistant Staphylococcus aureus assessed as inhibition of bacterial growth at 8 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID565498	Bactericidal activity against methicillin-resistant Staphylococcus aureus 6 on CAMHB media at 4 times MIC by time kill analysis	2009	Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10	In vitro bactericidal activity of iclaprim in human plasma.
AID556162	Antimicrobial activity against Clarithromycin-susceptible Streptococcus pneumoniae by broth microdilution method	2009	Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4	In vitro activity of Iclaprim against respiratory and bacteremic isolates of Streptococcus pneumoniae.
AID556171	Drug concentration in epithelial lining fluid of patient with Streptococcus pneumoniae infections at 1.6 mg/kg, iv administered as single 60 mins infusion measured after 5.5 to 7 hrs	2009	Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4	In vitro activity of Iclaprim against respiratory and bacteremic isolates of Streptococcus pneumoniae.
AID571772	Bactericidal activity against methicillin-resistant Staphylococcus aureus AW6 infected in in vitro human fibrin clot model assessed as log reduction in bacterial colony at 3.5 ug/ml after 24 hrs	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	Efficacy of iclaprim against wild-type and thymidine kinase-deficient methicillin-resistant Staphylococcus aureus isolates in an in vitro fibrin clot model.
AID556159	Antimicrobial activity against SXT-resistant Streptococcus pneumoniae by broth microdilution method	2009	Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4	In vitro activity of Iclaprim against respiratory and bacteremic isolates of Streptococcus pneumoniae.
AID561727	Antibacterial activity against Enterococcus faecium assessed as susceptible isolates by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID556167	Drug concentration in epithelial lining fluid of patient with Streptococcus pneumoniae infections at 1.6 mg/kg, iv administered as single 60 mins infusion measured after 1 to 2 hrs	2009	Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4	In vitro activity of Iclaprim against respiratory and bacteremic isolates of Streptococcus pneumoniae.
AID556158	Antimicrobial activity against SXT-susceptible Streptococcus pneumoniae by broth microdilution method	2009	Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4	In vitro activity of Iclaprim against respiratory and bacteremic isolates of Streptococcus pneumoniae.
AID561738	Antibacterial activity against Beta-hemolytic Streptococcus group A assessed as resistant isolates by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID556165	Antimicrobial activity against Doxycycline-susceptible Streptococcus pneumoniae by broth microdilution method	2009	Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4	In vitro activity of Iclaprim against respiratory and bacteremic isolates of Streptococcus pneumoniae.
AID565485	Bactericidal activity against methicillin-susceptible Staphylococcus aureus after 24 hrs by M26-A method	2009	Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10	In vitro bactericidal activity of iclaprim in human plasma.
AID561536	Antibacterial activity against Methicillin-resistant Staphylococcus aureus assessed as inhibition of bacterial growth at 0.25 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID561514	Antibacterial activity against Enterococcus faecalis by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID1074587	Inhibition of Staphylococcus aureus DHFR using dihydrofolate as substrate preincubated for 10 mins followed by substrate addition by spectrophotometric analysis in presence of NADPH	2014	Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3	Structure-based design of new dihydrofolate reductase antibacterial agents: 7-(benzimidazol-1-yl)-2,4-diaminoquinazolines.
AID561552	Antibacterial activity against Beta-hemolytic Streptococcus group A assessed as inhibition of bacterial growth at 0.5 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID1074572	Antibacterial activity against Streptococcus pneumoniae ATCC 700904 after 18 to 24 hrs by alamar Blue assay	2014	Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3	Structure-based design of new dihydrofolate reductase antibacterial agents: 7-(benzimidazol-1-yl)-2,4-diaminoquinazolines.
AID561342	Antibacterial activity against Beta-hemolytic Streptococcus group A by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID561560	Antibacterial activity against Beta-hemolytic Streptococcus group B assessed as inhibition of bacterial growth at <= 0.008 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID1074574	Antibacterial activity against Streptococcus pneumoniae ATCC 700677 after 18 to 24 hrs by alamar Blue assay	2014	Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3	Structure-based design of new dihydrofolate reductase antibacterial agents: 7-(benzimidazol-1-yl)-2,4-diaminoquinazolines.
AID614171	Ratio of Ki for human DHFR to Ki for Staphylococcus aureus DHFR	2011	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18	Structure-based design of new DHFR-based antibacterial agents: 7-aryl-2,4-diaminoquinazolines.
AID206647	Antibacterial activity against methicillin susceptible Staphylococcus aureus (MSSA)	2003	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23	Iclaprim, a novel diaminopyrimidine with potent activity on trimethoprim sensitive and resistant bacteria.
AID1074564	Antibacterial activity against Streptococcus pneumoniae after 18 to 24 hrs by alamar Blue assay	2014	Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3	Structure-based design of new dihydrofolate reductase antibacterial agents: 7-(benzimidazol-1-yl)-2,4-diaminoquinazolines.
AID561549	Antibacterial activity against Beta-hemolytic Streptococcus group A assessed as inhibition of bacterial growth at 0.06 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID565501	Bactericidal activity against methicillin-resistant Staphylococcus aureus 20 on CAMHB media at 4 times MIC by time kill analysis in presence of 50% human plasma	2009	Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10	In vitro bactericidal activity of iclaprim in human plasma.
AID561752	Antibacterial activity against Methicillin-resistant Staphylococcus aureus assessed as susceptible isolates by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID1074586	Inhibition of human DHFR using dihydrofolate as substrate preincubated for 10 mins followed by substrate addition by spectrophotometric analysis in presence of NADPH	2014	Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3	Structure-based design of new dihydrofolate reductase antibacterial agents: 7-(benzimidazol-1-yl)-2,4-diaminoquinazolines.
AID571776	Plasma protein binding in human	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	Efficacy of iclaprim against wild-type and thymidine kinase-deficient methicillin-resistant Staphylococcus aureus isolates in an in vitro fibrin clot model.
AID565491	Ratio of MBC to MIC for methicillin-susceptible Staphylococcus aureus in presence of 50% human plasma	2009	Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10	In vitro bactericidal activity of iclaprim in human plasma.
AID571550	Antimicrobial activity against methicillin-resistant Staphylococcus aureus AW6 grown on CAMHB media after 24 hrs by broth microdilution method in presence of 50% rat serum and 0.2 U/ml thymidine phosphorylase	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	Efficacy of iclaprim against wild-type and thymidine kinase-deficient methicillin-resistant Staphylococcus aureus isolates in an in vitro fibrin clot model.
AID571564	Protein binding in rat serum	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	Efficacy of iclaprim against wild-type and thymidine kinase-deficient methicillin-resistant Staphylococcus aureus isolates in an in vitro fibrin clot model.
AID561522	Antibacterial activity against Methicillin-sensitive Staphylococcus aureus assessed as inhibition of bacterial growth at 0.5 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID561516	Antibacterial activity against Methicillin-sensitive Staphylococcus aureus assessed as inhibition of bacterial growth at <= 0.008 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID571569	Bactericidal activity against thymidine kinase-deficient methicillin-resistant Staphylococcus aureus AH1252 assessed as loss of bacterial cell viability at 3.5 ug/ml measured within 8 hrs by time kill analysis in presence of 50% human serum	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	Efficacy of iclaprim against wild-type and thymidine kinase-deficient methicillin-resistant Staphylococcus aureus isolates in an in vitro fibrin clot model.
AID561724	Antibacterial activity against Enterococcus faecium assessed as resistant isolates by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID571773	Bactericidal activity against thymidine kinase-deficient methicillin-resistant Staphylococcus aureus AH1252 infected in in vitro human fibrin clot model assessed as log reduction in bacterial colony at 3.5 ug/ml after 24 hrs	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	Efficacy of iclaprim against wild-type and thymidine kinase-deficient methicillin-resistant Staphylococcus aureus isolates in an in vitro fibrin clot model.
AID1074585	Selectivity ratio of Ki for human DHFR to Ki for Staphylococcus aureus DHFR	2014	Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3	Structure-based design of new dihydrofolate reductase antibacterial agents: 7-(benzimidazol-1-yl)-2,4-diaminoquinazolines.
AID1074577	Antibacterial activity against Streptococcus pneumoniae ATCC 700671 after 18 to 24 hrs by alamar Blue assay	2014	Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3	Structure-based design of new dihydrofolate reductase antibacterial agents: 7-(benzimidazol-1-yl)-2,4-diaminoquinazolines.
AID614166	Antibacterial activity against ampicillin-resistant Haemophilus influenzae ATCC 49247 by CLSI microdilution method	2011	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18	Structure-based design of new DHFR-based antibacterial agents: 7-aryl-2,4-diaminoquinazolines.
AID561732	Antibacterial activity against Enterococcus faecalis assessed as inhibition of bacterial growth at 0.5 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID561563	Antibacterial activity against Beta-hemolytic Streptococcus group B assessed as inhibition of bacterial growth at 0.06 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID561564	Antibacterial activity against Beta-hemolytic Streptococcus group B assessed as inhibition of bacterial growth at 0.12 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID561745	Antibacterial activity against Methicillin-sensitive Staphylococcus aureus assessed as susceptible isolates by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID556156	Antimicrobial activity against Streptococcus pneumoniae isolated from respiratory tract of patient by broth microdilution method	2009	Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4	In vitro activity of Iclaprim against respiratory and bacteremic isolates of Streptococcus pneumoniae.
AID561747	Antibacterial activity against Methicillin-resistant Staphylococcus aureus assessed as resistant isolates by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID561515	Antibacterial activity against Enterococcus faecium by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID614168	Inhibition of Staphylococcus aureus DHFR assessed as oxidation of NADPH using dihydrofolate as substrate pre-incubated for 10 mins before substrate addition by spectrophotometry	2011	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18	Structure-based design of new DHFR-based antibacterial agents: 7-aryl-2,4-diaminoquinazolines.
AID57238	Inhibition of Escherichia coli dihydrofolate reductase (DHFR) enzyme by trimethoprim (TMP)	2003	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23	Iclaprim, a novel diaminopyrimidine with potent activity on trimethoprim sensitive and resistant bacteria.
AID561734	Antibacterial activity against Beta-hemolytic Streptococcus group B assessed as resistant isolates by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID565499	Bactericidal activity against methicillin-resistant Staphylococcus aureus 6 on CAMHB media at 4 times MIC by time kill analysis in presence of 50% human plasma	2009	Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10	In vitro bactericidal activity of iclaprim in human plasma.
AID565487	Bactericidal activity against methicillin-susceptible Staphylococcus aureus after 24 hrs by M26-A method in presence of 50% human plasma	2009	Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10	In vitro bactericidal activity of iclaprim in human plasma.
AID132398	Efficacy of compound to protect the methicillin resistant Staphylococcus aureus infected murine po administration	2003	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23	Iclaprim, a novel diaminopyrimidine with potent activity on trimethoprim sensitive and resistant bacteria.
AID561556	Antibacterial activity against Beta-hemolytic Streptococcus group A assessed as inhibition of bacterial growth at 8 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID556170	Drug concentration in alveolar macrophages of patient with Streptococcus pneumoniae infections at 1.6 mg/kg, iv administered as single 60 mins infusion measured after 5.5 to 7 hrs	2009	Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4	In vitro activity of Iclaprim against respiratory and bacteremic isolates of Streptococcus pneumoniae.
AID1074575	Antibacterial activity against Streptococcus pneumoniae ATCC 700675 after 18 to 24 hrs by alamar Blue assay	2014	Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3	Structure-based design of new dihydrofolate reductase antibacterial agents: 7-(benzimidazol-1-yl)-2,4-diaminoquinazolines.
AID561340	Antibacterial activity against Methicillin-sensitive Staphylococcus aureus by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID614167	Antibacterial activity against Escherichia coli ATCC 35218 by CLSI microdilution method	2011	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18	Structure-based design of new DHFR-based antibacterial agents: 7-aryl-2,4-diaminoquinazolines.
AID556161	Antimicrobial activity against penicillin-resistant Streptococcus pneumoniae by broth microdilution method	2009	Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4	In vitro activity of Iclaprim against respiratory and bacteremic isolates of Streptococcus pneumoniae.
AID571567	Bactericidal activity against thymidine kinase-deficient methicillin-resistant Staphylococcus aureus AH1252 assessed as loss of bacterial cell viability at 3.5 ug/ml by time kill analysis in presence of 50% rat serum	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	Efficacy of iclaprim against wild-type and thymidine kinase-deficient methicillin-resistant Staphylococcus aureus isolates in an in vitro fibrin clot model.
AID571548	Antimicrobial activity against methicillin-resistant Staphylococcus aureus AW6 grown on CAMHB media after 24 hrs by broth microdilution method in presence of 0.2 U/ml thymidine phosphorylase	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	Efficacy of iclaprim against wild-type and thymidine kinase-deficient methicillin-resistant Staphylococcus aureus isolates in an in vitro fibrin clot model.
AID561534	Antibacterial activity against Methicillin-resistant Staphylococcus aureus assessed as inhibition of bacterial growth at 0.06 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID556164	Antimicrobial activity against Ciprofloxacin-susceptible Streptococcus pneumoniae by broth microdilution method	2009	Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4	In vitro activity of Iclaprim against respiratory and bacteremic isolates of Streptococcus pneumoniae.
AID565481	Antimicrobial activity against methicillin-susceptible Staphylococcus aureus by broth microdilution method	2009	Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10	In vitro bactericidal activity of iclaprim in human plasma.
AID556160	Antimicrobial activity against penicillin-susceptible Streptococcus pneumoniae by broth microdilution method	2009	Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4	In vitro activity of Iclaprim against respiratory and bacteremic isolates of Streptococcus pneumoniae.
AID561531	Antibacterial activity against Methicillin-resistant Staphylococcus aureus assessed as inhibition of bacterial growth at <= 0.008 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID556163	Antimicrobial activity against Clarithromycin-resistant Streptococcus pneumoniae by broth microdilution method	2009	Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4	In vitro activity of Iclaprim against respiratory and bacteremic isolates of Streptococcus pneumoniae.
AID55685	Inhibition of Pneumocystis carinii dihydrofolate reductase (DHFR) enzyme by trimethoprim (TMP)	2003	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23	Iclaprim, a novel diaminopyrimidine with potent activity on trimethoprim sensitive and resistant bacteria.
AID1074583	Antibacterial activity against Staphylococcus aureus ATCC 13709 after 18 to 24 hrs by alamar Blue assay in presence of 20% heat inactivated mouse serum	2014	Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3	Structure-based design of new dihydrofolate reductase antibacterial agents: 7-(benzimidazol-1-yl)-2,4-diaminoquinazolines.
AID565497	Bactericidal activity against methicillin-resistant Staphylococcus aureus 3817 on CAMHB media at 4 times MIC by time kill analysis in presence of 50% human plasma	2009	Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10	In vitro bactericidal activity of iclaprim in human plasma.
AID556157	Antimicrobial activity against Streptococcus pneumoniae isolated from blood of patient by broth microdilution method	2009	Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4	In vitro activity of Iclaprim against respiratory and bacteremic isolates of Streptococcus pneumoniae.
AID561733	Antibacterial activity against Enterococcus faecalis assessed as inhibition of bacterial growth at 1 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID66125	Antibacterial activity against Enterococcus species	2003	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23	Iclaprim, a novel diaminopyrimidine with potent activity on trimethoprim sensitive and resistant bacteria.
AID561730	Antibacterial activity against Enterococcus faecalis assessed as inhibition of bacterial growth at 0.12 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID571553	Antimicrobial activity against methicillin-resistant Staphylococcus aureus AW6 grown on CAMHB media after 24 hrs by broth microdilution method in presence of 50% human serum and 0.2 U/ml thymidine phosphorylase	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	Efficacy of iclaprim against wild-type and thymidine kinase-deficient methicillin-resistant Staphylococcus aureus isolates in an in vitro fibrin clot model.
AID1074580	Antibacterial activity against Streptococcus pneumoniae ATCC 49619 after 18 to 24 hrs by alamar Blue assay	2014	Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3	Structure-based design of new dihydrofolate reductase antibacterial agents: 7-(benzimidazol-1-yl)-2,4-diaminoquinazolines.
AID571556	Antimicrobial activity against thymidine kinase-deficient methicillin-resistant Staphylococcus aureus AH1252 grown on CAMHB media after 24 hrs by broth microdilution method in presence of 0.2 U/ml thymidine phosphorylase	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	Efficacy of iclaprim against wild-type and thymidine kinase-deficient methicillin-resistant Staphylococcus aureus isolates in an in vitro fibrin clot model.
AID575159	Antimicrobial activity against methicillin-resistant Staphylococcus aureus	2010	Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9	Inhibition of antibiotic-resistant Staphylococcus aureus by the broad-spectrum dihydrofolate reductase inhibitor RAB1.
AID556168	Drug concentration in alveolar macrophages of patient with Streptococcus pneumoniae infections at 1.6 mg/kg, iv administered as single 60 mins infusion measured after 3 to 4 hrs	2009	Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4	In vitro activity of Iclaprim against respiratory and bacteremic isolates of Streptococcus pneumoniae.
AID561535	Antibacterial activity against Methicillin-resistant Staphylococcus aureus assessed as inhibition of bacterial growth at 0.12 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID571559	Antimicrobial activity against thymidine kinase-deficient methicillin-resistant Staphylococcus aureus AH1252 grown on CAMHB media after 24 hrs by broth microdilution method in presence of protein depleted rat serum	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	Efficacy of iclaprim against wild-type and thymidine kinase-deficient methicillin-resistant Staphylococcus aureus isolates in an in vitro fibrin clot model.
AID561758	Antibacterial activity against Enterococcus faecium assessed as inhibition of bacterial growth at 4 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID132399	Efficacy of compound to protect the methicillin resistant Staphylococcus pneumoniae infected murine sc administration	2003	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23	Iclaprim, a novel diaminopyrimidine with potent activity on trimethoprim sensitive and resistant bacteria.
AID561718	Antibacterial activity against Beta-hemolytic Streptococcus group B assessed as inhibition of bacterial growth at 8 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID575155	Inhibition of Staphylococcus aureus DHFR F98Y mutant by MTS assay	2010	Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9	Inhibition of antibiotic-resistant Staphylococcus aureus by the broad-spectrum dihydrofolate reductase inhibitor RAB1.
AID561341	Antibacterial activity against Methicillin-resistant Staphylococcus aureus by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID556166	Drug concentration in alveolar macrophages of patient with Streptococcus pneumoniae infections at 1.6 mg/kg, iv administered as single 60 mins infusion measured after 1 to 2 hrs	2009	Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4	In vitro activity of Iclaprim against respiratory and bacteremic isolates of Streptococcus pneumoniae.
AID571549	Antimicrobial activity against methicillin-resistant Staphylococcus aureus AW6 grown on CAMHB media after 24 hrs by broth microdilution method in presence of 50% rat serum	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	Efficacy of iclaprim against wild-type and thymidine kinase-deficient methicillin-resistant Staphylococcus aureus isolates in an in vitro fibrin clot model.
AID565483	Antimicrobial activity against methicillin-susceptible Staphylococcus aureus by broth microdilution method in presence of 50% human plasma	2009	Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10	In vitro bactericidal activity of iclaprim in human plasma.
AID561518	Antibacterial activity against Methicillin-sensitive Staphylococcus aureus assessed as inhibition of bacterial growth at 0.03 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID575154	Inhibition of Staphylococcus aureus wild type recombinant DHFR by MTS assay	2010	Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9	Inhibition of antibiotic-resistant Staphylococcus aureus by the broad-spectrum dihydrofolate reductase inhibitor RAB1.
AID561525	Antibacterial activity against Methicillin-sensitive Staphylococcus aureus assessed as inhibition of bacterial growth at 4 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID561533	Antibacterial activity against Methicillin-resistant Staphylococcus aureus assessed as inhibition of bacterial growth at 0.03 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID561753	Antibacterial activity against Enterococcus faecium assessed as inhibition of bacterial growth at 0.25 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID561520	Antibacterial activity against Methicillin-sensitive Staphylococcus aureus assessed as inhibition of bacterial growth at 0.12 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID561726	Antibacterial activity against Enterococcus faecalis assessed as resistant isolates by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID561513	Antibacterial activity against Beta-hemolytic Streptococcus group B by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID561736	Antibacterial activity against Beta-hemolytic Streptococcus group B assessed as susceptible isolates by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID561517	Antibacterial activity against Methicillin-sensitive Staphylococcus aureus assessed as inhibition of bacterial growth at 0.015 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID614170	Inhibition of human DHFR assessed as oxidation of NADPH using dihydrofolate as substrate pre-incubated for 10 mins before substrate addition by spectrophotometry	2011	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18	Structure-based design of new DHFR-based antibacterial agents: 7-aryl-2,4-diaminoquinazolines.
AID561759	Antibacterial activity against Enterococcus faecium assessed as inhibition of bacterial growth at 8 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID561748	Antibacterial activity against Enterococcus faecium assessed as inhibition of bacterial growth at 0.015 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID571565	Antimicrobial activity against methicillin-resistant Staphylococcus aureus AW6 grown on CAMHB media after 24 hrs by broth microdilution method in presence of 50% human serum and 1 ug/ml thymidine	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	Efficacy of iclaprim against wild-type and thymidine kinase-deficient methicillin-resistant Staphylococcus aureus isolates in an in vitro fibrin clot model.
AID561757	Antibacterial activity against Enterococcus faecium assessed as inhibition of bacterial growth at 2 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID571566	Bacteriostatic activity against methicillin-resistant Staphylococcus aureus AW6 assessed as loss of bacterial cell viability at 3.5 ug/ml by time kill analysis in presence of 50% rat serum	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	Efficacy of iclaprim against wild-type and thymidine kinase-deficient methicillin-resistant Staphylococcus aureus isolates in an in vitro fibrin clot model.
AID561561	Antibacterial activity against Beta-hemolytic Streptococcus group B assessed as inhibition of bacterial growth at 0.015 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID561731	Antibacterial activity against Enterococcus faecalis assessed as inhibition of bacterial growth at 0.25 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID561744	Antibacterial activity against Enterococcus faecalis assessed as inhibition of bacterial growth at >8 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID206822	Antibacterial activity against Staphylococcus pyogenes	2003	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23	Iclaprim, a novel diaminopyrimidine with potent activity on trimethoprim sensitive and resistant bacteria.
AID561539	Antibacterial activity against Methicillin-resistant Staphylococcus aureus assessed as inhibition of bacterial growth at 2 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID561755	Antibacterial activity against Methicillin-sensitive Staphylococcus aureus assessed as resistant isolates by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID561524	Antibacterial activity against Methicillin-sensitive Staphylococcus aureus assessed as inhibition of bacterial growth at 2 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID1074582	Antibacterial activity against TMP-resistant Staphylococcus aureus expressing DHFR F99Y mutant after 18 to 24 hrs by alamar Blue assay	2014	Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3	Structure-based design of new dihydrofolate reductase antibacterial agents: 7-(benzimidazol-1-yl)-2,4-diaminoquinazolines.
AID125103	Antibacterial activity against Moraxella catarrhalis	2003	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23	Iclaprim, a novel diaminopyrimidine with potent activity on trimethoprim sensitive and resistant bacteria.
AID571563	Protein binding in human serum	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	Efficacy of iclaprim against wild-type and thymidine kinase-deficient methicillin-resistant Staphylococcus aureus isolates in an in vitro fibrin clot model.
AID571560	Antimicrobial activity against thymidine kinase-deficient methicillin-resistant Staphylococcus aureus AH1252 grown on CAMHB media after 24 hrs by broth microdilution method in presence of 50% human serum	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	Efficacy of iclaprim against wild-type and thymidine kinase-deficient methicillin-resistant Staphylococcus aureus isolates in an in vitro fibrin clot model.
AID565492	Bactericidal activity against methicillin-susceptible Staphylococcus aureus ATCC 25923 on CAMHB media at 4 times MIC by time kill analysis	2009	Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10	In vitro bactericidal activity of iclaprim in human plasma.
AID565495	Bactericidal activity against methicillin-resistant Staphylococcus aureus 50478 on CAMHB media at 4 times MIC by time kill analysis in presence of 50% human plasma	2009	Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10	In vitro bactericidal activity of iclaprim in human plasma.
AID561565	Antibacterial activity against Beta-hemolytic Streptococcus group B assessed as inhibition of bacterial growth at 0.25 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID561551	Antibacterial activity against Beta-hemolytic Streptococcus group A assessed as inhibition of bacterial growth at 0.25 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID561537	Antibacterial activity against Methicillin-resistant Staphylococcus aureus assessed as inhibition of bacterial growth at 0.5 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID561521	Antibacterial activity against Methicillin-sensitive Staphylococcus aureus assessed as inhibition of bacterial growth at 0.25 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID561746	Antibacterial activity against Enterococcus faecium assessed as inhibition of bacterial growth at <= 0.008 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID565494	Bactericidal activity against methicillin-resistant Staphylococcus aureus 50478 on CAMHB media at 4 times MIC by time kill analysis	2009	Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10	In vitro bactericidal activity of iclaprim in human plasma.
AID561728	Antibacterial activity against Enterococcus faecalis assessed as inhibition of bacterial growth at 0.06 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID571552	Antimicrobial activity against methicillin-resistant Staphylococcus aureus AW6 grown on CAMHB media after 24 hrs by broth microdilution method in presence of 50% human serum	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	Efficacy of iclaprim against wild-type and thymidine kinase-deficient methicillin-resistant Staphylococcus aureus isolates in an in vitro fibrin clot model.
AID561749	Antibacterial activity against Enterococcus faecium assessed as inhibition of bacterial growth at 0.03 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID208756	Antibacterial activity against Streptococcus agalactiae	2003	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23	Iclaprim, a novel diaminopyrimidine with potent activity on trimethoprim sensitive and resistant bacteria.
AID561750	Antibacterial activity against Enterococcus faecium assessed as inhibition of bacterial growth at 0.06 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID561554	Antibacterial activity against Beta-hemolytic Streptococcus group A assessed as inhibition of bacterial growth at 2 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID565484	Bactericidal activity against methicillin-resistant Staphylococcus aureus after 24 hrs by M26-A method	2009	Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10	In vitro bactericidal activity of iclaprim in human plasma.
AID565482	Antimicrobial activity against methicillin-resistant Staphylococcus aureus by broth microdilution method in presence of 50% human plasma	2009	Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10	In vitro bactericidal activity of iclaprim in human plasma.
AID614163	Antibacterial activity against Staphylococcus aureus Smith ATCC 13709 by CLSI microdilution method	2011	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18	Structure-based design of new DHFR-based antibacterial agents: 7-aryl-2,4-diaminoquinazolines.
AID561739	Antibacterial activity against Enterococcus faecalis assessed as inhibition of bacterial growth at 8 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID1074579	Antibacterial activity against Streptococcus pneumoniae ATCC 700674 after 18 to 24 hrs by alamar Blue assay	2014	Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3	Structure-based design of new dihydrofolate reductase antibacterial agents: 7-(benzimidazol-1-yl)-2,4-diaminoquinazolines.
AID561725	Antibacterial activity against Enterococcus faecalis assessed as inhibition of bacterial growth at 0.03 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID565490	Ratio of MBC to MIC for methicillin-resistant Staphylococcus aureus in presence of 50% human plasma	2009	Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10	In vitro bactericidal activity of iclaprim in human plasma.
AID565480	Antimicrobial activity against methicillin-resistant Staphylococcus aureus by broth microdilution method	2009	Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10	In vitro bactericidal activity of iclaprim in human plasma.
AID208625	Antibacterial activity against Streptococcus pneumoniae (PEN-R)	2003	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23	Iclaprim, a novel diaminopyrimidine with potent activity on trimethoprim sensitive and resistant bacteria.
AID571551	Antimicrobial activity against methicillin-resistant Staphylococcus aureus AW6 grown on CAMHB media after 24 hrs by broth microdilution method in presence of protein depleted rat serum	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	Efficacy of iclaprim against wild-type and thymidine kinase-deficient methicillin-resistant Staphylococcus aureus isolates in an in vitro fibrin clot model.
AID561550	Antibacterial activity against Beta-hemolytic Streptococcus group A assessed as inhibition of bacterial growth at 0.12 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID561723	Antibacterial activity against Enterococcus faecalis assessed as inhibition of bacterial growth at 0.015 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID561526	Antibacterial activity against Methicillin-sensitive Staphylococcus aureus assessed as inhibition of bacterial growth at 8 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID571547	Antimicrobial activity against methicillin-resistant Staphylococcus aureus AW6 grown on CAMHB media after 24 hrs by broth microdilution method	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	Efficacy of iclaprim against wild-type and thymidine kinase-deficient methicillin-resistant Staphylococcus aureus isolates in an in vitro fibrin clot model.
AID571770	Bactericidal activity against thymidine kinase-deficient methicillin-resistant Staphylococcus aureus AH1252 infected in in vitro rat fibrin clot model assessed as reduction in bacterial colony at 3.5 ug/ml after 48 hrs	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	Efficacy of iclaprim against wild-type and thymidine kinase-deficient methicillin-resistant Staphylococcus aureus isolates in an in vitro fibrin clot model.
AID561523	Antibacterial activity against Methicillin-sensitive Staphylococcus aureus assessed as inhibition of bacterial growth at 1 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID561538	Antibacterial activity against Methicillin-resistant Staphylococcus aureus assessed as inhibition of bacterial growth at 1 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID571779	Bactericidal activity against methicillin-resistant Staphylococcus aureus AW6 at 3.5 ug/ml by time kill analysis in presence of 50% rat serum and 1 ug/ml thymidine	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	Efficacy of iclaprim against wild-type and thymidine kinase-deficient methicillin-resistant Staphylococcus aureus isolates in an in vitro fibrin clot model.
AID561729	Antibacterial activity against Enterococcus faecalis assessed as susceptible isolates by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID571562	Antimicrobial activity against thymidine kinase-deficient methicillin-resistant Staphylococcus aureus AH1252 grown on CAMHB media after 24 hrs by broth microdilution method in presence of protein depleted human serum	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	Efficacy of iclaprim against wild-type and thymidine kinase-deficient methicillin-resistant Staphylococcus aureus isolates in an in vitro fibrin clot model.
AID1074571	Antibacterial activity against Streptococcus pneumoniae ATCC BAA-255 after 18 to 24 hrs by alamar Blue assay	2014	Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3	Structure-based design of new dihydrofolate reductase antibacterial agents: 7-(benzimidazol-1-yl)-2,4-diaminoquinazolines.
AID561569	Antibacterial activity against Beta-hemolytic Streptococcus group B assessed as inhibition of bacterial growth at 4 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID571575	Bacteriostatic activity against methicillin-resistant Staphylococcus aureus AW6 infected in in vitro rat fibrin clot model assessed as reduction in bacterial colony at 3.5 ug/ml after 48 hrs	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	Efficacy of iclaprim against wild-type and thymidine kinase-deficient methicillin-resistant Staphylococcus aureus isolates in an in vitro fibrin clot model.
AID614172	Antibacterial activity against TMP-resistant Staphylococcus aureus harboring DHFR F99Y mutant by CLSI microdilution method	2011	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18	Structure-based design of new DHFR-based antibacterial agents: 7-aryl-2,4-diaminoquinazolines.
AID571561	Antimicrobial activity against thymidine kinase-deficient methicillin-resistant Staphylococcus aureus AH1252 grown on CAMHB media after 24 hrs by broth microdilution method in presence of 50% human serum and 0.2 U/ml thymidine phosphorylase	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	Efficacy of iclaprim against wild-type and thymidine kinase-deficient methicillin-resistant Staphylococcus aureus isolates in an in vitro fibrin clot model.
AID614164	Antibacterial activity against Staphylococcus aureus Smith ATCC 13709 in presence of 20% mouse serum by CLSI microdilution method	2011	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18	Structure-based design of new DHFR-based antibacterial agents: 7-aryl-2,4-diaminoquinazolines.
AID561547	Antibacterial activity against Beta-hemolytic Streptococcus group A assessed as inhibition of bacterial growth at 0.015 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID561735	Antibacterial activity against Enterococcus faecalis assessed as inhibition of bacterial growth at 2 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID614173	Inhibition of TMP-resistant Staphylococcus aureus DHFR F99Y mutant assessed as oxidation of NADPH using dihydrofolate as substrate pre-incubated for 10 mins before substrate addition by spectrophotometry	2011	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18	Structure-based design of new DHFR-based antibacterial agents: 7-aryl-2,4-diaminoquinazolines.
AID614169	Inhibition of Haemophilus influenzae DHFR assessed as oxidation of NADPH using dihydrofolate as substrate pre-incubated for 10 mins before substrate addition by spectrophotometry	2011	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18	Structure-based design of new DHFR-based antibacterial agents: 7-aryl-2,4-diaminoquinazolines.
AID565502	Plasma protein binding in human	2009	Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10	In vitro bactericidal activity of iclaprim in human plasma.
AID561555	Antibacterial activity against Beta-hemolytic Streptococcus group A assessed as inhibition of bacterial growth at 4 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID565489	Ratio of MBC to MIC for methicillin-susceptible Staphylococcus aureus	2009	Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10	In vitro bactericidal activity of iclaprim in human plasma.
AID56954	Inhibition of Human dihydrofolate reductase (DHFR) enzyme by Iclaprim	2003	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23	Iclaprim, a novel diaminopyrimidine with potent activity on trimethoprim sensitive and resistant bacteria.
AID55995	Inhibition of Staphylococcus aureus dihydrofolate reductase (DHFR) enzyme by trimethoprim (TMP)	2003	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23	Iclaprim, a novel diaminopyrimidine with potent activity on trimethoprim sensitive and resistant bacteria.
AID1074576	Antibacterial activity against Streptococcus pneumoniae ATCC 51916 after 18 to 24 hrs by alamar Blue assay	2014	Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3	Structure-based design of new dihydrofolate reductase antibacterial agents: 7-(benzimidazol-1-yl)-2,4-diaminoquinazolines.
AID561567	Antibacterial activity against Beta-hemolytic Streptococcus group B assessed as inhibition of bacterial growth at 1 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID565496	Bactericidal activity against methicillin-resistant Staphylococcus aureus 3817 on CAMHB media at 4 times MIC by time kill analysis	2009	Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10	In vitro bactericidal activity of iclaprim in human plasma.
AID614165	Antibacterial activity against Enterococcus faecalis ATCC 29212 by CLSI microdilution method	2011	Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18	Structure-based design of new DHFR-based antibacterial agents: 7-aryl-2,4-diaminoquinazolines.
AID561756	Antibacterial activity against Enterococcus faecium assessed as inhibition of bacterial growth at 1 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID1074573	Antibacterial activity against Streptococcus pneumoniae ATCC 700676 after 18 to 24 hrs by alamar Blue assay	2014	Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3	Structure-based design of new dihydrofolate reductase antibacterial agents: 7-(benzimidazol-1-yl)-2,4-diaminoquinazolines.
AID85783	Antibacterial activity against Haemophillia influenzae	2003	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23	Iclaprim, a novel diaminopyrimidine with potent activity on trimethoprim sensitive and resistant bacteria.
AID561754	Antibacterial activity against Enterococcus faecium assessed as inhibition of bacterial growth at 0.5 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID561546	Antibacterial activity against Beta-hemolytic Streptococcus group A assessed as inhibition of bacterial growth at <= 0.008 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID561562	Antibacterial activity against Beta-hemolytic Streptococcus group B assessed as inhibition of bacterial growth at 0.03 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID565488	Ratio of MBC to MIC for methicillin-resistant Staphylococcus aureus	2009	Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10	In vitro bactericidal activity of iclaprim in human plasma.
AID1074584	Antibacterial activity against Staphylococcus aureus ATCC 13709 after 18 to 24 hrs by alamar Blue assay	2014	Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3	Structure-based design of new dihydrofolate reductase antibacterial agents: 7-(benzimidazol-1-yl)-2,4-diaminoquinazolines.
AID571555	Antimicrobial activity against thymidine kinase-deficient methicillin-resistant Staphylococcus aureus AH1252 grown on CAMHB media after 24 hrs by broth microdilution method	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	Efficacy of iclaprim against wild-type and thymidine kinase-deficient methicillin-resistant Staphylococcus aureus isolates in an in vitro fibrin clot model.
AID132397	Efficacy of compound to protect the methicillin resistant Staphylococcus aureus infected murine iv administration	2003	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23	Iclaprim, a novel diaminopyrimidine with potent activity on trimethoprim sensitive and resistant bacteria.
AID561737	Antibacterial activity against Enterococcus faecalis assessed as inhibition of bacterial growth at 4 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID1074578	Antibacterial activity against Streptococcus pneumoniae ATCC 700669 after 18 to 24 hrs by alamar Blue assay	2014	Journal of medicinal chemistry, Feb-13, Volume: 57, Issue:3	Structure-based design of new dihydrofolate reductase antibacterial agents: 7-(benzimidazol-1-yl)-2,4-diaminoquinazolines.
AID571568	Bacteriostatic activity against methicillin-resistant Staphylococcus aureus AW6 assessed as loss of bacterial cell viability at 3.5 ug/ml measured within 8 hrs by time kill analysis in presence of 50% human serum	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	Efficacy of iclaprim against wild-type and thymidine kinase-deficient methicillin-resistant Staphylococcus aureus isolates in an in vitro fibrin clot model.
AID565493	Bactericidal activity against methicillin-susceptible Staphylococcus aureus ATCC 25923 on CAMHB media at 4 times MIC by time kill analysis in presence of 50% human plasma	2009	Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10	In vitro bactericidal activity of iclaprim in human plasma.
AID571777	Bactericidal activity against methicillin-resistant Staphylococcus aureus AW6 at 3.5 ug/ml by time kill analysis in presence of 50% human serum and 1 ug/ml thymidine	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	Efficacy of iclaprim against wild-type and thymidine kinase-deficient methicillin-resistant Staphylococcus aureus isolates in an in vitro fibrin clot model.
AID561740	Antibacterial activity against Beta-hemolytic Streptococcus group A assessed as susceptible isolates by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID571557	Antimicrobial activity against thymidine kinase-deficient methicillin-resistant Staphylococcus aureus AH1252 grown on CAMHB media after 24 hrs by broth microdilution method in presence of 50% rat serum	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	Efficacy of iclaprim against wild-type and thymidine kinase-deficient methicillin-resistant Staphylococcus aureus isolates in an in vitro fibrin clot model.
AID571570	Bactericidal activity against methicillin-resistant Staphylococcus aureus AW6 at 3.5 ug/ml by time kill analysis in presence of 50% rat serum and 0.2 U/ml thymidine phosphorylase	2009	Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9	Efficacy of iclaprim against wild-type and thymidine kinase-deficient methicillin-resistant Staphylococcus aureus isolates in an in vitro fibrin clot model.
AID561566	Antibacterial activity against Beta-hemolytic Streptococcus group B assessed as inhibition of bacterial growth at 0.5 ug/ml by CLSI broth microdilution method	2009	Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5	Potency and bactericidal activity of iclaprim against recent clinical gram-positive isolates.
AID565500	Bactericidal activity against methicillin-resistant Staphylococcus aureus 20 on CAMHB media at 4 times MIC by time kill analysis	2009	Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10	In vitro bactericidal activity of iclaprim in human plasma.
AID1797691	Enzyme Inhibition Assay from Article 10.1016/j.bmcl.2003.07.023: \\Iclaprim, a novel diaminopyrimidine with potent activity on trimethoprim sensitive and resistant bacteria.\\	2003	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 13, Issue:23	Iclaprim, a novel diaminopyrimidine with potent activity on trimethoprim sensitive and resistant bacteria.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	26 (57.78)	29.6817
2010's	17 (37.78)	24.3611
2020's	2 (4.44)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	7 (15.56%)	5.53%
Reviews	10 (22.22%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	28 (62.22%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Trial	Phase	Enrollment	Study Type	Start Date	Status
A Phase 3, Randomized, Double-blind, Multicenter Study to Evaluate the Safety and Efficacy of Intravenous Iclaprim Versus Vancomycin in the Treatment of ABSSSI: REVIVE-2 [NCT02607618]	Phase 3	613 participants (Actual)	Interventional	2015-11-30	Completed
Randomized, Double-Blind, Multicenter Study to Evaluate Efficacy and Safety of Intravenous Iclaprim Versus Vancomycin in the Treatment of Hospital-Acquired, Ventilator-Associated, or Health-Care-Associated Pneumonia Suspected or Confirmed to be Due to Gra [NCT00543608]	Phase 2	135 participants (Anticipated)	Interventional	2007-11-30	Terminated(stopped due to Trial terminated due to financial resource limitations)
Phase 3, Randomized, Investigator-Blind, Multi-Center Study to Evaluate Efficacy and Safety of Intravenous Iclaprim Versus Linezolid in Complicated Skin and Skin Structure Infections (ASSIST-2) [NCT00303550]	Phase 3	0 participants	Interventional	2006-03-31	Completed
Phase 3, Randomized, Investigator-Blind, Multi-Center Study to Evaluate Efficacy and Safety of Intravenous Iclaprim Versus Linezolid in Complicated Skin and Skin Structure Infections.(ASSIST-1) [NCT00299520]	Phase 3	0 participants	Interventional	2005-06-30	Completed
A Phase 3, Randomized, Double-blind, Multicenter Study to Evaluate the Safety and Efficacy of Intravenous Iclaprim Versus Vancomycin in the Treatment of ABSSSI: REVIVE-1 [NCT02600611]	Phase 3	600 participants (Actual)	Interventional	2015-11-01	Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial	Outcome
NCT02600611 (2) [back to overview]	≥20% Reduction in Lesion Size at 48 to 72 Hours Compared to Baseline in All Randomized Patients.
NCT02600611 (2) [back to overview]	Resolution or Near Resolution of Lesion at Test of Cure Visit
NCT02607618 (2) [back to overview]	Number of Participants With Resolution or Near Resolution of Lesion at Test of Cure Visit
NCT02607618 (2) [back to overview]	Percent of Participants With ≥20% Reduction in Lesion Size at 48 to 72 Hours Compared to Baseline

Intervention	percentage of participants (Number)
Iclaprim	80.9
Vancomycin	81.0

iclaprim

Description

Cross-References

Synonyms (51)

Research Excerpts

Overview

Effects

Treatment

Toxicity

Compound-Compound Interactions

Dosage Studied

Drug Classes (3)

Protein Targets (5)

Inhibition Measurements

Biological Processes (15)

Molecular Functions (12)

Ceullar Components (2)

Bioassays (205)

Research

Studies (45)

Market Indicators

Research Demand Index: 31.90

Study Types

Clinical Trials (5)

Trial Overview

Trial Outcomes

≥20% Reduction in Lesion Size at 48 to 72 Hours Compared to Baseline in All Randomized Patients.

Resolution or Near Resolution of Lesion at Test of Cure Visit

Number of Participants With Resolution or Near Resolution of Lesion at Test of Cure Visit

Percent of Participants With ≥20% Reduction in Lesion Size at 48 to 72 Hours Compared to Baseline

Substance	Relationship Strength	Studies	Trials	Classes	Roles
ciprofloxacin Ciprofloxacin: A broad-spectrum antimicrobial carboxyfluoroquinoline.. ciprofloxacin : A quinolone that is quinolin-4(1H)-one bearing cyclopropyl, carboxylic acid, fluoro and piperazin-1-yl substituents at positions 1, 3, 6 and 7, respectively.	2.74	3	0	aminoquinoline; cyclopropanes; fluoroquinolone antibiotic; N-arylpiperazine; quinolinemonocarboxylic acid; quinolone antibiotic; quinolone; zwitterion	antibacterial drug; antiinfective agent; antimicrobial agent; DNA synthesis inhibitor; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; environmental contaminant; topoisomerase IV inhibitor; xenobiotic
ofloxacin Ofloxacin: A synthetic fluoroquinolone antibacterial agent that inhibits the supercoiling activity of bacterial DNA GYRASE, halting DNA REPLICATION.. 9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid : An oxazinoquinoline that is 2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinolin-7-one substituted by methyl, carboxy, fluoro, and 4-methylpiperazin-1-yl groups at positions 3, 6, 9, and 10, respectively.. ofloxacin : A racemate comprising equimolar amounts of levofloxacin and dextrofloxacin. It is a synthetic fluoroquinolone antibacterial agent which inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication.	2.02	1	0	3-oxo monocarboxylic acid; N-arylpiperazine; N-methylpiperazine; organofluorine compound; oxazinoquinoline
trimethoprim Trimethoprim: A pyrimidine inhibitor of dihydrofolate reductase, it is an antibacterial related to PYRIMETHAMINE. It is potentiated by SULFONAMIDES and the TRIMETHOPRIM, SULFAMETHOXAZOLE DRUG COMBINATION is the form most often used. It is sometimes used alone as an antimalarial. TRIMETHOPRIM RESISTANCE has been reported.. trimethoprim : An aminopyrimidine antibiotic whose structure consists of pyrimidine 2,4-diamine and 1,2,3-trimethoxybenzene moieties linked by a methylene bridge.	8.68	9	0	aminopyrimidine; methoxybenzenes	antibacterial drug; diuretic; drug allergen; EC 1.5.1.3 (dihydrofolate reductase) inhibitor; environmental contaminant; xenobiotic
penicillin g Penicillin G: A penicillin derivative commonly used in the form of its sodium or potassium salts in the treatment of a variety of infections. It is effective against most gram-positive bacteria and against gram-negative cocci. It has also been used as an experimental convulsant because of its actions on GAMMA-AMINOBUTYRIC ACID mediated synaptic transmission.. benzylpenicillin : A penicillin in which the substituent at position 6 of the penam ring is a phenylacetamido group.	2.74	3	0	penicillin allergen; penicillin	antibacterial drug; drug allergen; epitope
methicillin Methicillin: One of the PENICILLINS which is resistant to PENICILLINASE but susceptible to a penicillin-binding protein. It is inactivated by gastric acid so administered by injection.. methicillin : A penicillin that is 6-aminopenicillanic acid in which one of the amino hydrogens is replaced by a 2,6-dimethoxybenzoyl group.	4.15	3	1	penicillin allergen; penicillin	antibacterial drug
oxacillin Oxacillin: An antibiotic similar to FLUCLOXACILLIN used in resistant staphylococci infections.. oxacillin : A penicillin antibiotic carrying a 5-methyl-3-phenylisoxazole-4-carboxamide group at position 6beta.	2.05	1	0	penicillin	antibacterial agent; antibacterial drug
ampicillin Ampicillin: Semi-synthetic derivative of penicillin that functions as an orally active broad-spectrum antibiotic.. ampicillin : A penicillin in which the substituent at position 6 of the penam ring is a 2-amino-2-phenylacetamido group.	2.05	1	0	beta-lactam antibiotic; penicillin allergen; penicillin	antibacterial drug
erythromycin Erythromycin: A bacteriostatic antibiotic macrolide produced by Streptomyces erythreus. Erythromycin A is considered its major active component. In sensitive organisms, it inhibits protein synthesis by binding to 50S ribosomal subunits. This binding process inhibits peptidyl transferase activity and interferes with translocation of amino acids during translation and assembly of proteins.. erythromycin : Any of several wide-spectrum macrolide antibiotics obtained from actinomycete Saccharopolyspora erythraea (formerly known as Streptomyces erythraeus).. erythromycin A : An erythromycin that consists of erythronolide A having 2,6-dideoxy-3-C-methyl-3-O-methyl-alpha-L-ribo-hexopyranosyl and 3,4,6-trideoxy-3-(dimethylamino)-beta-D-xylo-hexopyranosyl residues attahced at positions 4 and 6 respectively.	2.46	2	0	cyclic ketone; erythromycin
vancomycin Vancomycin: Antibacterial obtained from Streptomyces orientalis. It is a glycopeptide related to RISTOCETIN that inhibits bacterial cell wall assembly and is toxic to kidneys and the inner ear.. vancomycin : A complex glycopeptide from Streptomyces orientalis. It inhibits a specific step in the synthesis of the peptidoglycan layer in the Gram-positive bacteria Staphylococcus aureus and Clostridium difficile.	9.34	15	8	glycopeptide	antibacterial drug; antimicrobial agent; bacterial metabolite
cephalosporin c cephalosporin C: RN given refers to parent cpd; structure in Merck, 9th ed, #1937. cephalosporin C : A cephalosporin antibiotic carrying a 3-acetoxymethyl substituent and a 6-oxo-N(6)-L-lysino group at position 7.	5.7	6	0	cephalosporin	fungal metabolite
fropenem [no description available]	2.05	1	0	faropenem
2,4-diaminopyrimidine 2,6-diaminopyrimidine: structure in first source. pyrimidine-2,4-diamine : An aminopyrimidine in which a pyrimidine nucleus is substituted with amino groups at C-2 and C-4.	2.05	1	0	aminopyrimidine
doripenem Doripenem: A carbapenem derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of infections such as HOSPITAL-ACQUIRED PNEUMONIA, and complicated intra-abdominal or urinary-tract infections, including PYELONEPHRITIS.	4.69	3	0	carbapenems
oxazolidin-2-one Oxazolidinones: Derivatives of oxazolidin-2-one. They represent an important class of synthetic antibiotic agents.. oxazolidin-2-one : An oxazolidinone that is 1,3-oxazolidine with an oxo substituent at position 2.. oxazolidinone : An oxazolidine containing one or more oxo groups.	4.06	2	0	carbamate ester; oxazolidinone	metabolite
clarithromycin Clarithromycin: A semisynthetic macrolide antibiotic derived from ERYTHROMYCIN that is active against a variety of microorganisms. It can inhibit PROTEIN SYNTHESIS in BACTERIA by reversibly binding to the 50S ribosomal subunits. This inhibits the translocation of aminoacyl transfer-RNA and prevents peptide chain elongation.. clarithromycin : The 6-O-methyl ether of erythromycin A, clarithromycin is a macrolide antibiotic used in the treatment of respiratory-tract, skin and soft-tissue infections. It is also used to eradicate Helicobacter pylori in the treatment of peptic ulcer disease. It prevents bacteria from growing by interfering with their protein synthesis.	2.05	1	0	macrolide antibiotic	antibacterial drug; environmental contaminant; protein synthesis inhibitor; xenobiotic
methotrexate [no description available]	2.1	1	0	dicarboxylic acid; monocarboxylic acid amide; pteridines	abortifacient; antimetabolite; antineoplastic agent; antirheumatic drug; dermatologic drug; DNA synthesis inhibitor; EC 1.5.1.3 (dihydrofolate reductase) inhibitor; immunosuppressive agent
carbapenems [no description available]	4.69	3	0
beta-lactams 2-azetidinone: structure in first source. azetidin-2-one : An unsubstituted beta-lactam compound.. beta-lactam : A lactam in which the amide bond is contained within a four-membered ring, which includes the amide nitrogen and the carbonyl carbon.	3.55	2	0	beta-lactam antibiotic allergen; beta-lactam
levofloxacin Levofloxacin: The L-isomer of Ofloxacin.. levofloxacin : An optically active form of ofloxacin having (S)-configuration; an inhibitor of bacterial topoisomerase IV and DNA gyrase.	2.44	2	0	9-fluoro-3-methyl-10-(4-methylpiperazin-1-yl)-7-oxo-2,3-dihydro-7H-[1,4]oxazino[2,3,4-ij]quinoline-6-carboxylic acid; fluoroquinolone antibiotic; quinolone antibiotic	antibacterial drug; DNA synthesis inhibitor; EC 5.99.1.3 [DNA topoisomerase (ATP-hydrolysing)] inhibitor; topoisomerase IV inhibitor
ertapenem Ertapenem: A carbapenem derivative antibacterial agent that is more stable to renal dehydropeptidase I than IMIPENEM, but does not need to be given with an enzyme inhibitor such as CILASTATIN. It is used in the treatment of Gram-positive and Gram-negative bacterial infections including intra-abdominal infections, acute gynecological infections, complicated urinary tract infections, skin infections, and respiratory tract infections. It is also used to prevent infection in colorectal surgery.. ertapenem : Meropenem in which the one of the two methyl groups attached to the amide nitrogen is replaced by hydrogen while the other is replaced by a 3-carboxyphenyl group. The sodium salt is used for the treatment of moderate to severe susceptible infections including intra-abdominal and acute gynaecological infections, pneumonia, and infections of the skin and of the urinary tract.	3.15	1	0	carbapenemcarboxylic acid; pyrrolidinecarboxamide	antibacterial drug
temocillin temocillin: beta-lactam antibiotic with unusual spectrum of antibacterial activity & exceptional stability to bacterial beta-lactamases; RN given refers to di-Na salt (2S-(2alpha,5alpha,6alpha))-isomer; structure in first source. temocillin : A penicillin compound having a 6alpha-methoxy and 6beta-[2-carboxy(thiophen-3-yl)acetamido side-groups.	3.15	1	0	penicillin
trimethoprim, sulfamethoxazole drug combination Trimethoprim, Sulfamethoxazole Drug Combination: A drug combination with broad-spectrum antibacterial activity against both gram-positive and gram-negative organisms. It is effective in the treatment of many infections, including PNEUMOCYSTIS PNEUMONIA in AIDS.. co-trimoxazole : A two-component mixture comprising trimethoprim and sulfamethoxazole.	2.45	2	0
linezolid [no description available]	4.9	6	0	acetamides; morpholines; organofluorine compound; oxazolidinone	antibacterial drug; protein synthesis inhibitor
clindamycin Clindamycin: An antibacterial agent that is a semisynthetic analog of LINCOMYCIN.. clindamycin : A carbohydrate-containing antibiotic that is the semisynthetic derivative of lincomycin, a natural antibiotic.	2.46	2	0
zithromax Azithromycin: A semi-synthetic macrolide antibiotic structurally related to ERYTHROMYCIN. It has been used in the treatment of Mycobacterium avium intracellulare infections, toxoplasmosis, and cryptosporidiosis.. azithromycin : A macrolide antibiotic useful for the treatment of bacterial infections.	2.02	1	0	macrolide antibiotic	antibacterial drug; environmental contaminant; xenobiotic
nadp [no description available]	7.05	1	0
fusidic acid Fusidic Acid: An antibiotic isolated from the fermentation broth of Fusidium coccineum. (From Merck Index, 11th ed). It acts by inhibiting translocation during protein synthesis.. fusidic acid : A steroid antibiotic that is isolated from the fermentation broth of Fusidium coccineum.	2.05	1	0	11alpha-hydroxy steroid; 3alpha-hydroxy steroid; alpha,beta-unsaturated monocarboxylic acid; steroid acid; steroid antibiotic; sterol ester	EC 2.7.1.33 (pantothenate kinase) inhibitor; Escherichia coli metabolite; protein synthesis inhibitor
telavancin telavancin: an anti-infective agent; structure in first source. telavancin : A glycopeptide that is vancomycin substituted at position N-3'' by a 2-(decylamino)ethyl group and at position C-29 by a (phosphonomethyl)aminomethyl group. Used as its hydrochloride salt for treatment of adults with complicated skin and skin structure infections caused by bacteria.	5.09	5	0	glycopeptide	antibacterial drug; antimicrobial agent
gentamicin sulfate [no description available]	2.05	1	0
oritavancin oritavancin : A semisynthetic glycopeptide used (as its bisphosphate salt) for the treatment of acute bacterial skin and skin structure infections caused or suspected to be caused by susceptible isolates of designated Gram-positive microorganisms including MRSA.	4.57	4	0	disaccharide derivative; glycopeptide; semisynthetic derivative	antibacterial drug; antimicrobial agent
bc-3781 [no description available]	2.31	1	0
tetracycline Tetracycline: A naphthacene antibiotic that inhibits AMINO ACYL TRNA binding during protein synthesis.. tetracycline : A broad-spectrum polyketide antibiotic produced by the Streptomyces genus of actinobacteria.	2.46	2	0
minocycline Minocycline: A TETRACYCLINE analog, having a 7-dimethylamino and lacking the 5 methyl and hydroxyl groups, which is effective against tetracycline-resistant STAPHYLOCOCCUS infections.. minocycline : A tetracycline analogue having a dimethylamino group at position 7 and lacking the methyl and hydroxy groups at position 5.	4.06	2	0
tigecycline [no description available]	4.06	2	0
daptomycin [no description available]	4.06	2	0
ceftobiprole ceftobiprole: BAL5788 is Ceftobiprole medocaril sodium. ceftobiprole : A fifth-generation cephalosporin antibiotic having (E)-[(3'R)-2-oxo[1,3'-bipyrrolidin]-3-ylidene]methyl and [(2Z)-2-(5-amino-1,2,4-thiadiazol-3-yl)-2-(hydroxyimino)acetyl]amino side groups located at positions 3 and 7 respectively; developed for the treatment of hospital-acquired pneumonia (HAP, excluding ventilator-associated pneumonia, VAP) and community-acquired pneumonia (CAP).	5.34	5	0	cephalosporin; thiadiazoles	antimicrobial agent

Condition	Indicated	Relationship Strength	Studies	Trials
Blood Poisoning [description not available]	0	2.45	2	0
Sepsis Systemic inflammatory response syndrome with a proven or suspected infectious etiology. When sepsis is associated with organ dysfunction distant from the site of infection, it is called severe sepsis. When sepsis is accompanied by HYPOTENSION despite adequate fluid infusion, it is called SEPTIC SHOCK.	0	2.45	2	0
Bacteremia The presence of viable bacteria circulating in the blood. Fever, chills, tachycardia, and tachypnea are common acute manifestations of bacteremia. The majority of cases are seen in already hospitalized patients, most of whom have underlying diseases or procedures which render their bloodstreams susceptible to invasion.	0	2.05	1	0
Bacterial Infections, Gram-Positive [description not available]	0	8.05	7	2
Gram-Positive Bacterial Infections Infections caused by bacteria that retain the crystal violet stain (positive) when treated by the gram-staining method.	0	8.05	7	2
Infections, Staphylococcal [description not available]	0	9.5	8	4
Staphylococcal Infections Infections with bacteria of the genus STAPHYLOCOCCUS.	0	14.5	8	4
Infectious Skin Diseases [description not available]	0	5.35	4	1
Skin Diseases, Infectious Skin diseases caused by bacteria, fungi, parasites, or viruses.	0	5.35	4	1
Atypical Mycobacterial Infection, Disseminated [description not available]	0	2.31	1	0
Health Care Associated Infection [description not available]	0	4.79	2	1
Experimental Lung Inflammation Inflammation of any part, segment or lobe, of the lung parenchyma.	0	3.53	1	1
Cross Infection Any infection which a patient contracts in a health-care institution.	0	4.79	2	1
Pneumonia Infection of the lung often accompanied by inflammation.	0	8.53	1	1
Bacterial Pneumonia [description not available]	0	4.19	3	0
Pneumonia, Bacterial Inflammation of the lung parenchyma that is caused by bacterial infections.	0	4.19	3	0
Bacterial Skin Diseases [description not available]	0	10.62	10	7
Skin Diseases, Bacterial Skin diseases caused by bacteria.	0	10.62	10	7
Adverse Drug Event [description not available]	0	3.09	1	0
Drug-Related Side Effects and Adverse Reactions Disorders that result from the intended use of PHARMACEUTICAL PREPARATIONS. Included in this heading are a broad variety of chemically-induced adverse conditions due to toxicity, DRUG INTERACTIONS, and metabolic effects of pharmaceuticals.	0	3.09	1	0
Group A Strep Infection [description not available]	0	8.79	6	4
Acute Disease Disease having a short and relatively severe course.	0	8	5	5
Streptococcal Infections Infections with bacteria of the genus STREPTOCOCCUS.	0	8.79	6	4
Acute Kidney Failure [description not available]	0	2.17	1	0
Acute Kidney Injury Abrupt reduction in kidney function. Acute kidney injury encompasses the entire spectrum of the syndrome including acute kidney failure; ACUTE KIDNEY TUBULAR NECROSIS; and other less severe conditions.	0	7.17	1	0
Drug Abuse, Intravenous [description not available]	0	3.59	1	1
Infections, Staphylococcal Skin [description not available]	0	3.59	1	1
Staphylococcal Skin Infections Infections to the skin caused by bacteria of the genus STAPHYLOCOCCUS.	0	3.59	1	1
Bacterial Disease [description not available]	0	3.35	2	0
Bacterial Infections Infections by bacteria, general or unspecified.	1	5.35	2	0
Infections, Pseudomonas [description not available]	0	2.96	1	0
Pseudomonas Infections Infections with bacteria of the genus PSEUDOMONAS.	0	2.96	1	0
Infections, Soft Tissue [description not available]	0	2.96	1	0
Soft Tissue Infections Infections of non-skeletal tissue, i.e., exclusive of bone, ligaments, cartilage, and fibrous tissue. The concept is usually referred to as skin and soft tissue infections and usually subcutaneous and muscle tissue are involved. The predisposing factors in anaerobic infections are trauma, ischemia, and surgery. The organisms often derive from the fecal or oral flora, particularly in wounds associated with intestinal surgery, decubitus ulcer, and human bites. (From Cecil Textbook of Medicine, 19th ed, p1688)	0	7.96	1	0
Skin Diseases, Viral Skin diseases caused by viruses.	0	2.05	1	0
Infections, Chlamydia [description not available]	0	2.02	1	0
Chlamydia Infections Infections with bacteria of the genus CHLAMYDIA.	0	2.02	1	0
Infections, Legionella pneumophila [description not available]	0	2.03	1	0

iclaprim

Description

Cross-References

Synonyms (51)

Research Excerpts

Overview

Effects

Treatment

Toxicity

Compound-Compound Interactions

Dosage Studied

Drug Classes (3)

Protein Targets (5)

Inhibition Measurements

Biological Processes (15)

Molecular Functions (12)

Ceullar Components (2)

Bioassays (205)

Research

Studies (45)

Market Indicators

Research Demand Index: 31.90

Study Types

Clinical Trials (5)

Trial Overview

Trial Outcomes

≥20% Reduction in Lesion Size at 48 to 72 Hours Compared to Baseline in All Randomized Patients.

Resolution or Near Resolution of Lesion at Test of Cure Visit

Number of Participants With Resolution or Near Resolution of Lesion at Test of Cure Visit

Percent of Participants With ≥20% Reduction in Lesion Size at 48 to 72 Hours Compared to Baseline

Related Drugs (36)

Related Conditions (38)